公开(公告)号：US20240285772A1

公开(公告)日：2024-08-29

申请号：US18106242

申请日：2023-02-06

申请人： University of Rhode Island Board of Trustees ,  Colgate University

发明人： Fang Wang ,  Jacob M. Goldberg ,  Bradley M. Lipka ,  Daniel S. Honeycutt

IPC分类号： A61K47/54 ,  C07D213/61 ,  C07D213/64 ,  C07D213/68 ,  C07D213/71 ,  C07D213/76 ,  C07D235/24 ,  C07D235/28 ,  C07D237/12 ,  C07D239/30 ,  C07D277/62

CPC分类号： A61K47/545 ,  C07D213/61 ,  C07D213/64 ,  C07D213/68 ,  C07D213/71 ,  C07D213/76 ,  C07D235/24 ,  C07D235/28 ,  C07D237/12 ,  C07D239/30 ,  C07D277/62

摘要： Disclosed are pnictogen-containing heterocyclic compounds of Formula (I)




Each of R1, the heterocyclic ring H, A+, LG, and X− is defined herein. Also provided are methods of modifying a substrate using such a compound, conjugated biomolecules thus modified, and pharmaceutical compositions containing one of the conjugated biomolecules.

公开(公告)号：US11952389B2

公开(公告)日：2024-04-09

申请号：US17735258

申请日：2022-05-03

申请人： Enanta Pharmaceuticals, Inc.

发明人： Brian C. Shook ,  In Jong Kim ,  Thomas P. Blaisdell ,  Jianming Yu ,  Joseph D. Panarese ,  Yat Sun Or

IPC分类号： C07D235/24 ,  A61K31/5513 ,  A61K31/56 ,  A61K31/58 ,  A61K45/06 ,  A61P31/14 ,  A61P31/16 ,  C07D243/16 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D491/048 ,  C07D495/04 ,  C07D498/08 ,  C07D513/04

CPC分类号： C07D513/04 ,  A61K31/5513 ,  A61K31/56 ,  A61K31/58 ,  A61K45/06 ,  C07D243/16 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D491/048 ,  C07D495/04 ,  C07D498/08 ,  A61K31/5513 ,  A61K2300/00 ,  A61K31/58 ,  A61K2300/00 ,  A61K31/56 ,  A61K2300/00

摘要： The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:




which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

公开(公告)号：US20230303489A1

公开(公告)日：2023-09-28

申请号：US17982187

申请日：2022-11-07

申请人： Aquinnah Pharmaceuticals, Inc.

发明人： Duane A. Burnett ,  Joseph P. Vacca

IPC分类号： C07D209/42 ,  C07D235/24 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

CPC分类号： C07D209/42 ,  C07D235/24 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

摘要： Herein, compounds, compositions and methods for modulating inclusion formation and stress granules in cells related to the onset of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmological diseases, and viral infections are described.

公开(公告)号：US11634404B2

公开(公告)日：2023-04-25

申请号：US16093365

申请日：2017-04-14

申请人： The United States of America, as represented by the Secretary, Department of Health and Human Services ,  The University of Kansas ,  The University of North Carolina at Chapel Hill

发明人： David R. Sibley ,  Amy Elizabeth Moritz ,  R. Benjamin Free ,  Joseph P. Steiner ,  Noel Terrence Southall ,  Marc Ferrer ,  Xin Hu ,  Warren S. Weiner ,  Jeffrey Aubé ,  Kevin Frankowski

IPC分类号： C07D401/12 ,  A61P25/28 ,  C07D295/185 ,  C07D209/42 ,  C07D213/65 ,  C07D213/81 ,  C07D235/24 ,  C07D307/85 ,  C07D317/64 ,  C07D333/70 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04

摘要： The disclosure of a compound of Formula (I) or a pharmaceutically acceptable salt thereof (I) The variables W, R1, R2, R3, and R4 are defined in the disclosure. The disclosure provides a compound or salt of Formula (I) together with a pharmaceutically acceptable carrier. The disclosure also provides methods of treating a patient for Parkinson's disease and related syndromes, dyskinesia, especially dyskinesias secondary to treating Parkinson's disease with L-DOPA, neurodegenerative disorders such as Alzheimer's disease and dementia, Huntington's disease, restless legs syndrome, bipolar disorder and depression, schizophrenia, cognitive dysfunction, or substance use disorders, the methods comprising administering a compound of Formula I or salt thereof to the patient. The disclosure provides combination methods of treatment in which the compound of Formula (I) is administered to the patient together with one or more additional active agents.

公开(公告)号：US11572475B2

公开(公告)日：2023-02-07

申请号：US14233044

申请日：2012-07-18

申请人： Maged Henary ,  W. David Wilson

发明人： Maged Henary ,  W. David Wilson

IPC分类号： C09B23/06 ,  C07D209/14 ,  C07D403/06 ,  C07D213/73 ,  C07D209/49 ,  C07D403/12 ,  C07D407/12 ,  C07D249/10 ,  C07D231/14 ,  C07D413/14 ,  C07D239/34 ,  C07D231/20 ,  C07D401/14 ,  C07D401/04 ,  C07D403/10 ,  C07D209/18 ,  C07D235/24 ,  C07D417/12 ,  C07D213/64

摘要： Cyanines which selectively bind to G-quadruplex DNA complexes, particularly quadruplexes expressed in cancer cells, and methods of making and using thereof are described herein. The cyanine can be a symmetrical or unsymmetrical streptocyanine, hemicyanine, closed chain cyanine, or combinations thereof. The cyanine is preferably substituted with one or more groups that minimize or prevent aggregation of the cyanine and/or inhibit binding of the cyanine to duplex DNA. One or more of the cyanines can be formulated with one or more pharmaceutical excipients and/or carrier to prepare pharmaceutical compositions suitable for administration to a patient, particular a human patient. The compounds and compositions described herein can be used to treat diseases or disorders characterized by the expression of G-quadruplex DNA, such as cancer.

公开(公告)号：US20220304984A1

公开(公告)日：2022-09-29

申请号：US17618829

申请日：2020-06-12

申请人： VANDERBILT UNIVERSITY

发明人： H. Charles Manning ,  Michael Schulte

IPC分类号： A61K31/42 ,  C07D209/42 ,  C07D307/85 ,  C07D333/70 ,  C07D235/24 ,  C07D263/58 ,  C07D277/68 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D487/04 ,  C07D473/00 ,  C07D207/34 ,  C07D333/40 ,  C07D307/68 ,  C07D231/20 ,  C07D275/03 ,  C07D261/18 ,  C07D233/90 ,  C07D277/56 ,  C07D263/40 ,  C07D249/12 ,  C07D285/08 ,  C07D271/07 ,  C07D285/13 ,  C07D271/113 ,  A61K45/06 ,  A61K31/404 ,  A61K31/343 ,  A61K31/381 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/519 ,  A61K31/52 ,  A61K31/401 ,  A61K31/341 ,  A61K31/415 ,  A61K31/425 ,  A61K31/4164 ,  A61K31/426 ,  A61K31/421 ,  A61K31/4196 ,  A61K31/433 ,  A61K31/4245

摘要： These compounds are glutamine transporter inhibitors, e.g., alanine, serine, cysteine-preferring transporter 2 (ASCT2) inhibitors. Glutamine transporter inhibitors are useful to treat a variety of diseases, disorders, or conditions including cancer.

公开(公告)号：US20200299285A1

公开(公告)日：2020-09-24

申请号：US16825561

申请日：2020-03-20

申请人： University of Maryland, Baltimore

发明人： Steven Fletcher ,  Brandon Drennen

IPC分类号： C07D413/12 ,  C07D231/56 ,  C07D235/24 ,  C07D405/12 ,  C07D401/12 ,  C07D403/12

摘要： Mcl-1 selective inhibitors, Bcl-2 selective inhibitors, and Mcl-1/Bcl-2 dual inhibitors and methods of using the same for the treatment of disease are disclosed.

公开(公告)号：US20200270211A1

公开(公告)日：2020-08-27

申请号：US16472501

申请日：2017-12-22

申请人： Aquinnah Pharmaceuticals, Inc.

发明人： Duane A. Burnett ,  Joseph P. Vacca

IPC分类号： C07D209/42 ,  C07D471/04 ,  C07D235/24 ,  C07D405/12 ,  C07D413/12

摘要： Herein, compounds, compositions and methods for modulating inclusion formation and stress granules in cells related to the onset of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmological diseases, and viral infections are described.

公开(公告)号：US20190367486A1

公开(公告)日：2019-12-05

申请号：US16295476

申请日：2019-03-07

申请人： Janssen Pharmaceutica NV

发明人： Frances Meredith Hocutt ,  Barry Eastman Leonard, JR. ,  Hillary M. Peltier ,  Victor K. Phuong ,  Michael H. Rabinowitz ,  Mark D. Rosen ,  Kyle T. Tarantino ,  Hariharan Venkatesan ,  Lucy Xiumin Zhao

IPC分类号： C07D403/04 ,  C07D487/04 ,  C07D403/14 ,  C07D235/24 ,  C07D513/04 ,  C07D473/40 ,  C07D471/04

摘要： The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.

公开(公告)号：US20190269683A1

公开(公告)日：2019-09-05

申请号：US16258024

申请日：2019-01-25

申请人： Vertex Pharmaceuticals Incorporated

发明人： Mark Thomas Miller ,  Corey Anderson ,  Vijayalaksmi Arumugam ,  Brian Richard Bear ,  Haley Marie Binch ,  Jeremy J. Clemens ,  Thomas Cleveland ,  Erica Conroy ,  Timothy Richard Coon ,  Bryan A. Frieman ,  Peter Diederik Jan Grootenhuis ,  Raymond Stanley Gross ,  Sara Sabina Hadida-Ruah ,  Haripada Khatuya ,  Pramod Virupax Joshi ,  Paul John Krenitsky ,  Chun-Chieh Lin ,  Gulin Erdogan Marelius ,  Vito Melillo ,  Jason McCartney ,  Georgia McGaughey Nicholls ,  Fabrice Jean Denis Pierre ,  Alina Silina ,  Andreas P. Termin ,  Johnny Uy ,  Jinglan Zhou

IPC分类号： A61K31/506 ,  A61K31/4525 ,  C07D403/12 ,  A61K31/4709 ,  A61K31/4545 ,  C07D405/14 ,  C07D417/12 ,  A61K31/497 ,  C07D231/12 ,  C07D401/14 ,  A61K31/4439 ,  C07D401/12 ,  A61K31/404 ,  C07D209/42 ,  A61K31/415 ,  C07D231/14 ,  C07D213/84 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4418 ,  C07D213/82 ,  A61J1/03 ,  C07D213/64 ,  C07D209/49 ,  C07D209/18 ,  C07D407/12 ,  C07D239/34 ,  C07D403/10 ,  C07D235/24 ,  C07D401/04 ,  C07D231/20 ,  C07D213/73 ,  C07D413/14 ,  A61K31/496

摘要： The present invention features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, R3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.